Concepedia

A New Generation of Specific <i>Trypanosoma cruzi trans</i>‐Sialidase Inhibitors

Sabrina Buchini, Alejandro Buschiazzo, Stephen G. Withers

Angewandte Chemie International Edition · 2008 · 87 citations · 7 references

DOI

Concepts

Abstract

A substitution for inhibition: The incorporation of an aryl substituent at C9 of 3-fluorosialyl fluorides provides specificity and dramatically slows the reactivation of the glycosylphosphatidylinositol-anchored surface protein Trypanosoma cruzi trans-sialidase (TcTS) by transglycosylation (see picture). X-ray crystallographic analysis of the trapped intermediate has provided a structural rationale for this behavior.

References

7

The Genome Sequence of <i>Trypanosoma cruzi</i> , Etiologic Agent of Chagas Disease

Najib M. El-Sayed, Peter J. Myler, Daniella Castanheira Bartholomeu et al. · Science · 2005 · 1.4K citations · Full text

, , +17

Investigating Cellular Metabolism of Synthetic Azidosugars with the Staudinger Ligation

Eliana Saxon, Sarah J. Luchansky, Howard C. Hang et al. · Journal of the American Chemical Society · 2002 · 301 citations

, , +14

The Crystal Structure and Mode of Action of Trans-Sialidase, a Key Enzyme in Trypanosoma cruzi Pathogenesis

Alejandro Buschiazzo, M.F. Amaya, María Laura Cremona et al. · Molecular Cell · 2002 · 244 citations · Full text

, , +15

<i>Trypanosoma c</i><i>ruzi</i> Trans-sialidase Operates through a Covalent Sialyl−Enzyme Intermediate:  Tyrosine Is the Catalytic Nucleophile

Andrew G. Watts, Iben Damager, Maria L. Amaya et al. · Journal of the American Chemical Society · 2003 · 209 citations

, , +17

Structural Insights into the Catalytic Mechanism of Trypanosoma cruzi trans-Sialidase

M.F. Amaya, Andrew G. Watts, Iben Damager et al. · Structure · 2004 · 208 citations

, , +14